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首页> 外文期刊>Medicinal chemistry >Synthesis, structural characterization and antibacterial activity of novel 7beta-{(3-(substituted phenyl)-2-propenoyl)amino}-3-((2,5-dihydro-6-hydroxy-2-methyl)-5-oxo-cis-triazin- 3-yl)-thiomethyl-cefalosporins.
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Synthesis, structural characterization and antibacterial activity of novel 7beta-{(3-(substituted phenyl)-2-propenoyl)amino}-3-((2,5-dihydro-6-hydroxy-2-methyl)-5-oxo-cis-triazin- 3-yl)-thiomethyl-cefalosporins.

机译：新型7β-{（3-（取代苯基）-2-丙烯酰基）氨基} -3-（（2,5-二氢-6-羟基-2-甲基）-5-氧代-的合成，结构表征和抗菌活性顺式-三嗪-3-基）-硫代甲基头孢菌素。

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摘要

A series of 3-[(2,5-dihydro-6-hydroxy-2-methyl)-5-oxo-cis-triazin-3-yl]-thiomethyl-cefalospor ins with various 3-phenyl-2-propenoyl substituted groups at the 7beta-position were synthesized, structurally characterized and evaluated for antibacterial activity in vitro. To prepare these derivatives by the Vilsmeier's reagent method, it was necessary to carefully control the reaction conditions in order to avoid the formation of the biologically inactive alpha epimer. The NMR studies showed that the 3-phenyl-2-propenoyl moiety has little effect on chemical shifts of cephem nucleus protons and carbon atoms. Some of these cephalosporin derivatives showed good in vitro activity against methicillin sensible strains of Staphylococcus aureus (MSSA) and coagulase negative Staphylococcus (MSCoNS). Particularly effective were the compounds carrying a 3-(2'-chlorophenyl)-2-propenoyl or 2-methyl-3-phenyl-2-propenoyl moiety at 7beta-position, both with an antibacterial potency close to cefazoline and higher than cefuroxime. All the synthesized cephalosporins were inactive against methicillin resistant strains of Staphylococcus aureus (MRSA) and coagulase negative Staphylococcus (MRCoNS).
机译：具有各种3-苯基-2-丙烯酰基取代基的一系列3-[（2,5-二氢-6-羟基-2-甲基）-5-氧代-顺-三嗪-3-基]-硫代甲基头孢菌素合成了7β-位的β-内酰胺酶，对其结构进行了表征并评估了其体外抗菌活性。为了通过维尔斯迈尔试剂法制备这些衍生物，必须小心地控制反应条件，以避免形成生物学上无活性的α差向异构体。 NMR研究表明3-苯基-2-丙烯酰基部分对头孢烯核质子和碳原子的化学位移影响很小。这些头孢菌素衍生物中的一些对甲氧西林敏感的金黄色葡萄球菌（MSSA）和凝固酶阴性葡萄球菌（MSCoNS）表现出良好的体外活性。特别有效的是在7β位带有3-（2'-氯苯基）-2-丙烯酰基或2-甲基-3-苯基-2-丙烯酰基部分的化合物，其抗菌效力均接近头孢唑啉且高于头孢呋辛。所有合成的头孢菌素均对耐甲氧西林的金黄色葡萄球菌（MRSA）和凝固酶阴性葡萄球菌（MRCoNS）无活性。

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